反应详情

Ethyl 2-(1-methyl-4-(N-(4-octylphenyl)sulfamoylamino)piperidin-4-yl)acetate (39 mg, 0.084 mmol), was treated with MeI (0.2 mL, 3.2 mmol) as described in example 2a to yield crude 4-(2-ethoxy-2-oxoethyl)-1,1-dimethyl-4-(N-(4-octylphenyl)sulfamoyl-amino)piperidinium iodide which was used without further purification. Subsequent saponification and preparative HPLC purification gave the title compound (8 mg, 17%) as white solid. 1H NMR (400 MHz, CD3OD) δ 7.20 (d, 2H, J=8.4 Hz), 7.15 (d, 2H, J=8.8 Hz), 3.27-3.15 (m, 4H), 3.08 (s, 3H), 2.88 (s, 2H), 2.81 (s, 3H), 2.59 (t, 2H, J=15.6 Hz), 2.39 (d, 2H, J=15.6 Hz), 2.26-2.18 (m, 2H), 1.65-1.55 (m, 2H), 1.48-1.25 (m, 10H), 0.91 (t, 3H, J=6.8 Hz); MS ESI 454.3 [M+H]+, calcd for [C23H39N3O4S+H]+ 454.27.